IL248948B - - α3hydroxy--β3-methoxymethyl-5)-21-methyl-2h-tetrazole-2-yl-19-nor-α5-paragnane-20-one and its pharmaceutical preparation - Google Patents

- α3hydroxy--β3-methoxymethyl-5)-21-methyl-2h-tetrazole-2-yl-19-nor-α5-paragnane-20-one and its pharmaceutical preparation

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Publication number
IL248948B
IL248948B IL248948A IL24894816A IL248948B IL 248948 B IL248948 B IL 248948B IL 248948 A IL248948 A IL 248948A IL 24894816 A IL24894816 A IL 24894816A IL 248948 B IL248948 B IL 248948B
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IL
Israel
Prior art keywords
mmol
compound
solution
added
synthesis
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Application number
IL248948A
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English (en)
Hebrew (he)
Other versions
IL248948A0 (en
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Sage Therapeutics Inc
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Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of IL248948A0 publication Critical patent/IL248948A0/en
Publication of IL248948B publication Critical patent/IL248948B/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL248948A 2014-05-29 2015-05-29 - α3hydroxy--β3-methoxymethyl-5)-21-methyl-2h-tetrazole-2-yl-19-nor-α5-paragnane-20-one and its pharmaceutical preparation IL248948B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2014078820 2014-05-29
PCT/CN2015/080216 WO2015180679A1 (en) 2014-05-29 2015-05-29 Neuroactive steroids, compositions, and uses thereof

Publications (2)

Publication Number Publication Date
IL248948A0 IL248948A0 (en) 2017-01-31
IL248948B true IL248948B (en) 2022-09-01

Family

ID=54698130

Family Applications (3)

Application Number Title Priority Date Filing Date
IL248948A IL248948B (en) 2014-05-29 2015-05-29 - α3hydroxy--β3-methoxymethyl-5)-21-methyl-2h-tetrazole-2-yl-19-nor-α5-paragnane-20-one and its pharmaceutical preparation
IL292461A IL292461B2 (en) 2014-05-29 2015-05-29 3?-hydroxy-3?-methoxymethyl-21-(5-methyl-2h-tetrazol-2-yl)-19-nor-5?-pregnan-20-one for use in a method of treating cns-related disorders
IL304033A IL304033A (en) 2014-05-29 2015-05-29 Neuroactive steroids, preparations and their uses

Family Applications After (2)

Application Number Title Priority Date Filing Date
IL292461A IL292461B2 (en) 2014-05-29 2015-05-29 3?-hydroxy-3?-methoxymethyl-21-(5-methyl-2h-tetrazol-2-yl)-19-nor-5?-pregnan-20-one for use in a method of treating cns-related disorders
IL304033A IL304033A (en) 2014-05-29 2015-05-29 Neuroactive steroids, preparations and their uses

Country Status (27)

Country Link
US (7) US20180179247A1 (de)
EP (3) EP3705488B1 (de)
JP (4) JP6652934B2 (de)
KR (3) KR20240066304A (de)
CN (3) CN114369135A (de)
AR (2) AR100691A1 (de)
AU (5) AU2015266447A1 (de)
CA (2) CA3279948A1 (de)
CY (1) CY1124109T1 (de)
DK (2) DK3705488T3 (de)
ES (2) ES2805598T3 (de)
HR (2) HRP20221294T1 (de)
HU (2) HUE059829T2 (de)
IL (3) IL248948B (de)
JO (1) JO3691B1 (de)
LT (2) LT3705488T (de)
MX (5) MX394493B (de)
PH (2) PH12021550762A1 (de)
PL (2) PL3705488T3 (de)
PT (2) PT3705488T (de)
RS (2) RS60529B1 (de)
RU (2) RU2019126637A (de)
SG (2) SG10201803812TA (de)
SI (2) SI3705488T1 (de)
SM (2) SMT202000406T1 (de)
TW (3) TW201625661A (de)
WO (1) WO2015180679A1 (de)

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TW202604538A (zh) 2016-08-23 2026-02-01 美商賽吉醫療公司 結晶19-去甲c3,3-二取代之c21-n-吡唑類固醇
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SG10201803812TA (en) 2018-06-28
AU2021204410A1 (en) 2021-07-22
MX2016015532A (es) 2017-02-27
NZ764941A (en) 2023-11-24
KR102664412B1 (ko) 2024-05-21
NZ726260A (en) 2023-11-24
AR100691A1 (es) 2016-10-26
RU2019126637A (ru) 2019-10-03
AR121661A2 (es) 2022-06-29
SI3149018T1 (sl) 2020-10-30
US20260116911A1 (en) 2026-04-30
ES2927007T3 (es) 2022-10-31
IL292461B1 (en) 2023-11-01
ES2805598T3 (es) 2021-02-12
SG11201609813XA (en) 2016-12-29
HRP20221294T1 (hr) 2023-03-03
CY1124109T1 (el) 2022-03-24
JP7863073B2 (ja) 2026-05-20
US20210061850A1 (en) 2021-03-04
TW202426001A (zh) 2024-07-01
JO3691B1 (ar) 2020-08-27
IL248948A0 (en) 2017-01-31
RU2016151727A (ru) 2018-07-02
MX2023004352A (es) 2023-05-08
RU2699359C2 (ru) 2019-09-05
SI3705488T1 (sl) 2022-10-28
US20200165291A1 (en) 2020-05-28
PL3705488T3 (pl) 2022-12-05
EP4144746A1 (de) 2023-03-08
SMT202200416T1 (it) 2022-11-18
HRP20201126T1 (hr) 2020-12-11
HUE059829T2 (hu) 2022-12-28
IL292461A (en) 2022-06-01
EP3705488B1 (de) 2022-08-03
TWI839649B (zh) 2024-04-21
PH12016502342A1 (en) 2017-02-13
HUE050028T2 (hu) 2021-12-28
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WO2015180679A1 (en) 2015-12-03
JP7386204B2 (ja) 2023-11-24
DK3149018T3 (da) 2020-07-20
PH12021550762A1 (en) 2023-07-17
MX394493B (es) 2025-03-24
KR102494061B1 (ko) 2023-01-31
CN114133423A (zh) 2022-03-04
LT3705488T (lt) 2022-09-26
EP3705488A1 (de) 2020-09-09
IL304033A (en) 2023-08-01
CN114369135A (zh) 2022-04-19
SMT202000406T1 (it) 2020-09-10
JP2023123878A (ja) 2023-09-05
MX382131B (es) 2025-03-13
PT3705488T (pt) 2022-09-30
RS63554B1 (sr) 2022-09-30
US20240076310A1 (en) 2024-03-07
KR20230021165A (ko) 2023-02-13
US20260116912A1 (en) 2026-04-30
JP6892936B2 (ja) 2021-06-23
EP3149018B1 (de) 2020-04-29
CA3279948A1 (en) 2025-10-31
AU2023285755A1 (en) 2024-01-18
CA2949720C (en) 2025-11-18
CN106661078A (zh) 2017-05-10
EP3149018A1 (de) 2017-04-05
US20180179247A1 (en) 2018-06-28
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IL292461B2 (en) 2024-03-01
TW201625661A (zh) 2016-07-16
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JP2021130696A (ja) 2021-09-09
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AU2019279910A1 (en) 2020-01-16
MX2021005099A (es) 2021-06-15
KR20170003706A (ko) 2017-01-09
BR112016027508A2 (pt) 2018-06-26
PT3149018T (pt) 2020-07-21
NZ764921A (en) 2023-11-24
RU2016151727A3 (de) 2018-12-03
LT3149018T (lt) 2020-08-10
AU2023285755B2 (en) 2026-03-12
RS60529B1 (sr) 2020-08-31
AU2021204410B2 (en) 2023-09-21
CA2949720A1 (en) 2015-12-03
US20210061849A1 (en) 2021-03-04
AU2026201227A1 (en) 2026-03-12
TW202231652A (zh) 2022-08-16
EP3149018A4 (de) 2017-12-06
DK3705488T3 (da) 2022-10-03
JP2020073577A (ja) 2020-05-14
JP2017516793A (ja) 2017-06-22
MX2021005106A (es) 2021-06-15

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